MLN-1117
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MedKoo CAT#: 205743

CAS#: 1268454-23-4

Description: Serabelisib (also known as MLN1117, INK1117, and TAK-117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. PI3K alpha inhibitor INK1117 selectively inhibits PI3K alpha kinase, including mutations of PIK3CA, in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K alpha-expressing tumor cells. By specifically targeting class I PI3K alpha, this agent may be more efficacious and less toxic than pan-PI3K inhibitors.


Price and Availability

Size
Price

10mg
USD 120
100mg
USD 550
1g
USD 2950
Size
Price

25mg
USD 190
200mg
USD 950
2g
USD 3950
Size
Price

50mg
USD 350
500mg
USD 1850
5g
Ask price

Serabelisib (MLN1117, INK1117, TAK-117), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international). Note: the estimated shipping out time for order > 500mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205743
Name: MLN-1117
CAS#: 1268454-23-4
Chemical Formula: C19H17N5O3
Exact Mass: 363.1331
Molecular Weight: 363.377
Elemental Analysis: C, 62.80; H, 4.72; N, 19.27; O, 13.21


Synonym: INK1117; INK-1117; INK 1117; MLN1117; MLN 1117; MLN-1117; TAK-117; TAK 117; TAK117; Serabelisib

IUPAC/Chemical Name: [6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-methanone

InChi Key: BLGWHBSBBJNKJO-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17N5O3/c20-19-22-14-9-12(1-3-16(14)27-19)13-2-4-17-21-10-15(24(17)11-13)18(25)23-5-7-26-8-6-23/h1-4,9-11H,5-8H2,(H2,20,22)

SMILES Code: O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5


Technical Data

Appearance:
Brown solid powder

Purity:
>98%

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

INK1117 has demonstrated significant efficacy in several PI3Kα mutant-specific preclinical mouse xenograft tumor models. Moreover, daily oral administration of INK1117 inhibited tumor growth in a dose-dependent manner with a predicted PK/PD relationship, was well tolerated at a range of efficacious doses, and exhibited several differentiating features from less selective inhibitors that target the PI3K/Akt/mTOR pathway.  A Phase I dose escalation study is underway to evaluate the safety, tolerability and pharmacokinetics of single-agent INK1117 in patients with advanced solid malignancies who have tumors characterized by the presence of a PIK3CA mutation.   (source: http://www.intellikine.com/pipeline/pi3kalpha_inhibitors.html).
 
 
 


References

1: Yea SS, So L, Mallya S, Lee J, Rajasekaran K, Malarkannan S, Fruman DA.
Effects of novel isoform-selective phosphoinositide 3-kinase inhibitors on
natural killer cell function. PLoS One. 2014 Jun 10;9(6):e99486. doi:
10.1371/journal.pone.0099486. eCollection 2014. PubMed PMID: 24915189; PubMed
Central PMCID: PMC4051752.

2: So L, Yea SS, Oak JS, Lu M, Manmadhan A, Ke QH, Janes MR, Kessler LV,
Kucharski JM, Li LS, Martin MB, Ren P, Jessen KA, Liu Y, Rommel C, Fruman DA.
Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte
function. J Biol Chem. 2013 Feb 22;288(8):5718-31. doi: 10.1074/jbc.M112.379446.
Epub 2012 Dec 28. PubMed PMID: 23275335; PubMed Central PMCID: PMC3581375.